Urinary pharmacokinetics of methamphetamine and its metabolite, amphetamine following controlled oral administration to humans
Urinary pharmacokinetics of methamphetamine and its metabolite, amphetamine following controlled oral administration to humans
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DOI：
10.1097/00007691-200412000-00013
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发表时间：
2004-12-01
影响因子：
2.5
通讯作者：
Huestis, MA
中科院分区：
文献类型：
--
作者：
Kim, I;Oyler, JM;Huestis, MA
甲基安非他明因其令人欣快的作用而被广泛滥用。我们的目标是描述甲基苯丙胺和苯丙胺的尿液药代动力学控制甲基苯丙胺管理后，以改善尿液药物检测结果的解释。参与者（n = 8）在7天内接受4次每日10 mg（低）口服剂量的缓释（d）-甲基苯丙胺盐酸盐。4周后，5名参与者接受4次每日20 mg（高）口服剂量。在研究期间采集所有尿液标本。甲基苯丙胺和苯丙胺通过GC-MS/PCI测量。甲基苯丙胺的最大排泄率范围为403至4919 mug/h，苯丙胺为59至735 mug/h，剂量与排泄率之间无关系。尿液中总甲基苯丙胺和苯丙胺剂量的平均摩尔百分比分别为57.5 +/- 21.7%（低剂量）和40.9 +/- 8.5%（高剂量）。不同剂量的甲基苯丙胺和苯丙胺的平均尿终末消除半衰期分别为23.6 +/- 6.6小时和20.7 +/- 7.3小时。各剂量甲基苯丙胺肾清除率为175 - 102 mL/min。平均苯丙胺/甲基苯丙胺百分比比的基础上，尿排泄-时间曲线下面积随时间增加，从13.4 +/- 6.5%至35.7 +/-26.6%。缓慢的尿液排泄导致药物蓄积和检测时间窗增加。我们的研究结果也支持存在一个活跃的肾脏排泄机制的甲基苯丙胺。
Methamphetamine is widely abused for its euphoric effects. Our objectives were to characterize the urinary pharmacokinetics of methamphetamine and amphetamine after controlled methamphetamine administration to humans and to improve the interpretation of urine drug test results. Participants (n = 8) received 4 daily 10-mg (low) oral doses of sustained-re lease (d)-methamphetamine hydrochloride within 7 days. After 4 weeks, 5 participants received 4 daily 20-mg (high) oral doses. All urine specimens were collected during the study. Methamphetamine and amphetamine were measured by GC-MS/PCI. Maximum excretion rates ranged from 403 to 4919 mug/h for methamphetamine and 59 to 735 mug/h for amphetamine with no relationship between dose and excretion rate. The mean molar percentage of dose in the urine as total methamphetamine and amphetamine were 57.5 +/- 21.7% (low dose) and 40.9 +/- 8.5% (high dose). Mean urinary terminal elimination half-lives across doses were 23.6 +/- 6.6 hours for methamphetamine and 20.7 +/- 7.3 hours for amphetamine. Methamphetamine renal clearance across doses was 175 102 mL/min. The mean amphetamine/methamphetamine percentage ratio based on the area under the urinary excretion-time curve increased over time from 13.4 +/- 6.5% to 35.7 +/- 26.6%. Slow urinary excretion results in drug accumulation and increases in detection time windows. Our findings also support the presence of an active renal excretion mechanism for methamphetamine.